CN105456234A - Novel propellant asarone inhalation aerosol and preparation method thereof - Google Patents
Novel propellant asarone inhalation aerosol and preparation method thereof Download PDFInfo
- Publication number
- CN105456234A CN105456234A CN201410461968.4A CN201410461968A CN105456234A CN 105456234 A CN105456234 A CN 105456234A CN 201410461968 A CN201410461968 A CN 201410461968A CN 105456234 A CN105456234 A CN 105456234A
- Authority
- CN
- China
- Prior art keywords
- inhalation aerosol
- asarone
- asarin
- propellant
- preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Abstract
The invention discloses a novel propellant asarone inhalation aerosol and a preparation method. The asarone inhalation aerosol is prepared from, by mass, asarone, a propellant, cosolvent, an antioxidant, corrigent and a bacteriostatic agent, wherein hydrofluoroalkane (HFA) is adopted as the propellant. A preparation technology of the asarone inhalation aerosol is high in industrialization level, and meanwhile the bioavailability of the asarone inhaled through the mouth is improved. The asarone inhalation aerosol effectively solves the problems that the bioavailability is low if the asarone is taken orally, and an asarone injection is serious in toxic and side effects, has the advantages of being capable of quickly achieving the effects, convenient to use, convenient to carry due to small size and the like and can be clinically and widely applied to asthma, inflammation resisting, cough relieving, phlegm eliminating and asthma relieving.
Description
Technical field
The invention belongs to medical art, more specifically relate to a kind of alpha-ararin inhalation aerosol and preparation method thereof.
Technical background
Asthma is called as worldwide disease, and the global strategy of asthma control is pointed out in guilding principle for 2007, and there is the asthmatic patient of about 300,000,000 in the whole world.From 1%-18% not etc., and sickness rate is still constantly increasing the sickness rate of asthma in countries in the world.The number nearly 250,000 of the annual death because of asthma in the whole world.According to investigations, in the state-owned asthmatic patient more than 2,000 ten thousand, the sickness rate of asthma is about 2.0%, and in the trend that rises year by year; The treating asthma measure of China and means also comparatively backwardness, asthma mortality rate is about 4/10000ths, occupies the first place of global asthma mortality rate.
Chronic obstructive pulmonary disease (be called for short COPD): be the disease that is feature with not exclusively reversible flow limitation.The flow limitation development in Progressive symmetric erythrokeratodermia usually, and react relevant with the abnormal inflammatory of lung to the deleterious particles such as smoke from cigarette or gas.COPD is a kind of global chronic disease and the cause of death, has nowadays become the 4th of the global cause of death.According to World Health Organization's statistics, the whole world about has 2.1 hundred million people's suffering from copd altogether.2005, the whole world about had 3,000,000 people to die from COPD, is equivalent to 5% of death toll then.Point out according to chronic obstructive pulmonary disease in China diagnosis and treatment guide (revised edition in 2007), Chinese COPD prevalence accounts for more than 40 years old crowd's 8.2%, and the height of its prevalence is very surprising.
At present, China's asthma, COPD patient altogether more than 7,000 ten thousand people, and reach more than 7,500,000,000 yuans for the pharmaceutical market capacity for the treatment of.And along with China's economic development, the continuation in the environment short time worsens, and as the continuous rising of PM2.5, the sickness rate of asthma, COPD all can be made to increase.But it is different that China sucks preparation (comprising Foradil Aerolizer formoterol fumarate and inhalation aerosol) when treating these diseases with external main use, the theophylline series of the still oral or drug administration by injection that China's dosage is maximum, has most the inhalation kind of rescuing meaning also not popularized to asthma.
Asarone (Asarone) has another name called α asarone or α-asaricin, chemical name Alpha-Asaronum, be Chinese medicine Rhizoma Acori Graminei mainly contain one of effective constituent.From the sixties, both at home and abroad asarone was both conducted extensive research, confirm that it has very strong pharmacologically active, tool calmness, cough-relieving, eliminate the phlegm, relieving asthma, spasmolytic and anticonvulsant action, also have inhibitory action in various degree to Diplococcus pneumoniae, staphylococcus aureus and colibacillary growth.Be mainly used in the treatment of bronchial asthma, chronic bronchitis, pneumonia and chronic obstructive pulmonary disease companion pulmonary acute inflammation etc. clinically.
Asarone is domestic unique Chinese medicine monomer synthesis antiinflammatory expelling phlegm for arresting cough antiasthmatics, and more obvious than the cough-relieving Zhichuan effect of pure Chinese medicinal preparation, the Western medicine preparation in chemosynthesis compares therapeutic effect better, and without any toxicity, side effect.
Medicinal substances extract or fine drug powder and suitable propellant are contained in by aerosol (aerosol) to be had in the withstand voltage tight envelope container of special valve system, makes content with the preparation of fine mist or the ejection of other forms during use by the pressure of propellant.Inhalation aerosol (inhalationaerosol) is divided into: refer to that content is vaporific ejection and sucks the aerosol of pulmonary by the used time by route of administration.Inhalation aerosol also can be divided into unit dose package or multiple-unit container.2) non-inhalation aerosol: the used time is directly sprayed onto the aerosol of tract mucosa (oral cavity, nasal cavity, vagina etc.).(3) aerosol for external use: refer to the aerosol for skin and space disinfection
Inhalation aerosol has the irreplaceable advantage of other dosage forms, occupies certain status in clinical treatment.The advantage of aerosol mainly comprises: 1. have quick-acting and positioning action, and the aerosol as treated asthma can make drug particle directly enter pulmonary, and sucking 2min can be effective; 2. medicine is enclosed within that medicine to be kept to clean in container aseptic, because container is light tight, does not directly contact with the oxygen in air in moisture, because this increasing the stability of medicine; 3. medicine can avoid gastrointestinal to destroy regulating liver-QI first pass effect through pulmonary absorption; 4. anapnotherapy is the gold therapy of asthma and chronic obstructive pulmonary disease; 5. use quantitative valve can accurate control dose; 6. easy to use.
Although aerosol has above-mentioned advantage, for the indissoluble feature of different principal agent asarone, and select the difficulties such as suitable adjuvant, still there is no the good Asarin inhalation aerosol product of effect in the market.
The research starting of China on inhalation aerosol is late, and the market of current most domestic is all captured by foreign medicine.What the domestic aerosol of China used is mostly that dichlorodifluoromethan hydro carbons (also known as freon) is as propellant, it is low that this kind of propellant has boiling point, easy to control, stable in properties, nonflammable, tasteless, basic odorless, toxicity is less, water insoluble, can make the advantages such as the solvent of fat-soluble medicine, be desirable medicinal propellant.But because fluorochloroparaffins is to the destruction of atmospheric ozone layer, WHO has required to stop using.China determines aerosol dichlorodifluoromethan hydro carbons to be time of inessential purposes be December in 2015 31 days.
Ejecting agent hydrofluoroalkane (HFA) its character, boiling point and low boiling freon are similar, but its chemical stability is poor, and polarity is less.And due to HFA and freon difference in physicochemical property very remarkable, traditional freon preparation technique can not simply be transplanted to HFA dosage form.
Summary of the invention
The present invention is directed to above-mentioned existing problems, provide a kind of new administering mode alpha-ararin inhalation aerosol, it has good stability, and toxic and side effects is little, uses feature easy to carry, by the direct pulmonary administration of respiratory tract.
The technical scheme realizing above-mentioned purpose is as follows:
A kind of alpha-ararin inhalation aerosol, it is made up of the raw material of following weight parts:
Described propellant is hydrofluoroalkane (HFA).
Preferably, the weight portion of above-mentioned alpha-ararin is 0.5-2.0 part, and the weight portion of described propellant is 8.5-9.5 part.
Another object of the present invention is the preparation method that there are provided a kind of above-mentioned alpha-ararin inhalation aerosol, and this preparation method is simple, easy to operate.
In order to realize above-mentioned object, the present invention adopts following technical measures:
A preparation method for above-mentioned Asarin inhalation aerosol, its step comprises:
A, cosolvent, correctives, antioxidant, antibacterial are mixed to dissolving;
B, the solution in same A to be added in pressure vessel together;
C, gained in step B plugged in valve, envelope valve, propellant fill containing the pressure vessel of medicine, to obtain final product.
Preferably, described cosolvent is ethanol, glycerol wherein a kind of or their mixing.
Described correctives is citric acid, tartaric acid, cyclamate, sucralose, xylitol, fructose, Oleum Cinnamomi, oleum Citri sinensis, menthol, flavoring orange essence, Fructus Citri Limoniae volatile oil wherein a kind of or their mixture.
Described antioxidant is butylated hydroxyarisol (BHA), two fourth cresols (BHT), tocopherol wherein a kind of or their mixture
Described antibacterial is methyl hydroxybenzoate, ethyl hydroxybenzoate wherein a kind of or their mixture
The present invention compared with the existing technology has the following advantages:
1) described alpha-ararin inhalation aerosol good stability, dosage is accurate, uses simple, easy to carry, patient's better tolerance.It is by the direct administration of pulmonary, and can arrive patient lungs rapidly, avoid first pass effect, decrease side effect, local concentration is high, and medicine is better played a role in vivo.
2) described alpha-ararin inhalation aerosol adopts pressure vessel aluminium pot, keeps in Dark Place, the stability of medicine is improved greatly.Relative oral and injection asarone, this product carries simply, easy to use.
3) by experience and the great many of experiments of the accumulation of inventor, select most suitable propellant and relevant proportioning, described alpha-ararin inhalation aerosol can not need other adjuvants such as cosolvent, and good stability, toxic and side effects can be reduced and make preparation method more simple and reliable.
Detailed description of the invention
Set forth Asarin inhalation aerosol of the present invention further by the following examples.
Embodiment 1:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds medicine:
The preparation method of above-mentioned Asarin inhalation aerosol, the steps include:
A, claim tartaric acid, two fourth cresols, methyl hydroxybenzoate to join in glycerol by weight, be stirred to dissolving;
B, the asarone in formula to be added in pressure vessel, and add the solution of step A;
C, loading onto gained in step B valve containing the pressure vessel of medicine and tightening, press-in HFA, to obtain final product.
Embodiment 2:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Raw material weight (g)
Alpha-ararin 0.5
HFA-134a9.5。
The preparation method of described Asarin inhalation aerosol, the steps include:
A, the asarone in formula is added in pressure vessel;
B, valve loaded onto and tightens, press-in HFA, both.
Embodiment 3:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following mass parts raw material:
Its preparation process is identical with embodiment 1.
Embodiment 4:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Its preparation process is identical with embodiment 1.
Embodiment 5:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Its preparation process is identical with embodiment 1.
Embodiment 6:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Embodiment 7:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Raw materials quality (g)
Alpha-ararin 0.5
HFA-134a9.5。
Its preparation process is identical with embodiment 2.
Embodiment 8:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Its preparation process is identical with embodiment 1.
Embodiment 9:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Its preparation process is identical with embodiment 1.
Embodiment 10:
Suck Asarin inhalation aerosol described in the present embodiment, it is made up of following quality feeds:
Its preparation process is identical with embodiment 1.
Embodiment 11: stability study
The proportioning of the Asarin inhalation aerosol described in above-described embodiment 1-10 is carried out to the stability test of the room temperature of 100 days, asarone having good stability in HFA.
By formula preparation asarone aerosol, obtained asarone aerosol is kept in Dark Place 100 days at normal temperatures.
Visual inspection: examine under aerosol being placed in light.
Outward appearance: the Asarin inhalation aerosol solution described in embodiment 1-10 keeps clear always.
Claims (7)
1. an Asarin inhalation aerosol, is characterized in that, it is made up of the supplementary material material of following mass parts:
Described propellant is hydrofluoroalkane (HFA).
2. Asarin inhalation aerosol according to claim 1, is characterized in that, the mass parts of described alpha-ararin is 0.5-2.0 part, and the weight portion of described propellant is 8.5-10 part.
3. Asarin inhalation aerosol according to claim 1, is characterized in that, described cosolvent is ethanol, glycerol wherein a kind of or their mixing.
4. Asarin inhalation aerosol according to claim 1, it is characterized in that, described correctives is citric acid, tartaric acid, cyclamate, sucralose, xylitol, fructose, Oleum Cinnamomi, oleum Citri sinensis, menthol, flavoring orange essence, Fructus Citri Limoniae volatile oil wherein a kind of or their mixture.
5. Asarin inhalation aerosol according to claim 1, is characterized in that, described antioxidant is butylated hydroxyarisol (BHA), two fourth cresols (BHT), tocopherol wherein a kind of or their mixture.
6. Asarin inhalation aerosol according to claim 1, is characterized in that, described antibacterial is methyl hydroxybenzoate, ethyl hydroxybenzoate wherein a kind of or their mixture.
7. prepare a method for Asarin inhalation aerosol described in any one of claim 1-6, the steps include:
A, by cosolvent, correctives, antioxidant, antibacterial mixing or mix to dissolving;
B, the solution in same A to be added in pressure vessel together;
C, gained in step B plugged in valve, envelope valve, propellant fill containing the pressure vessel of medicine, both.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410461968.4A CN105456234A (en) | 2014-09-12 | 2014-09-12 | Novel propellant asarone inhalation aerosol and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410461968.4A CN105456234A (en) | 2014-09-12 | 2014-09-12 | Novel propellant asarone inhalation aerosol and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105456234A true CN105456234A (en) | 2016-04-06 |
Family
ID=55594702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410461968.4A Pending CN105456234A (en) | 2014-09-12 | 2014-09-12 | Novel propellant asarone inhalation aerosol and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105456234A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105998079A (en) * | 2016-05-13 | 2016-10-12 | 齐鲁工业大学 | Preparation technology of lumbricus aerosol |
| CN114522143A (en) * | 2022-02-22 | 2022-05-24 | 暨南大学 | Low-refrigeration-effect composite propellant for inhalation aerosol and preparation method and application thereof |
| CN114796166A (en) * | 2021-01-29 | 2022-07-29 | 北京远大九和药业有限公司 | Aerosol containing terpene volatile oil and preparation method thereof |
-
2014
- 2014-09-12 CN CN201410461968.4A patent/CN105456234A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105998079A (en) * | 2016-05-13 | 2016-10-12 | 齐鲁工业大学 | Preparation technology of lumbricus aerosol |
| CN114796166A (en) * | 2021-01-29 | 2022-07-29 | 北京远大九和药业有限公司 | Aerosol containing terpene volatile oil and preparation method thereof |
| CN114522143A (en) * | 2022-02-22 | 2022-05-24 | 暨南大学 | Low-refrigeration-effect composite propellant for inhalation aerosol and preparation method and application thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2767062C2 (en) | Compositions, devices and methods for the treatment of alcohol dependence | |
| RU2014140674A (en) | NEW DOSAGE AND DRUG FORM | |
| EP2908834B1 (en) | New formulations comprising plant extracts | |
| EP3932400A1 (en) | Peramivir solution type inhalant and preparation method therefor | |
| AU2015261104A1 (en) | Combinations of formoterol and budesonide for the treatment of COPD | |
| WO2019119720A1 (en) | Fudosteine solution preparation for aerosol inhalation, and preparation method therefor | |
| CN105456234A (en) | Novel propellant asarone inhalation aerosol and preparation method thereof | |
| CN109512880A (en) | A kind of sucking preparation and preparation method thereof, application | |
| CN102335132A (en) | Asarin inhalation aerosol and preparation method thereof | |
| ES2601860T3 (en) | Effervescent tablets for inhalation use | |
| EP2821062A1 (en) | Novel dry powder inhaler formulations | |
| WO2019091082A1 (en) | Solution preparation for aerosol inhalation of carbocisteine, and preparation method therefor | |
| CN102512676A (en) | Methods of using a thiazole derivative | |
| CN103462942A (en) | Suction-type ambroxol hydrochloride solution | |
| US9782368B2 (en) | Use of N,N-bis-2-mercaptoethyl isophthalamide | |
| CN110755413B (en) | Ambroxol hydrochloride solution for inhalation and preparation method thereof | |
| RU2519653C1 (en) | Aerosol preparation of ipratropium bromide for treating respiratory diseases | |
| CN114344380A (en) | Asthma-relieving aerosol inhalation solution preparation and preparation method thereof | |
| CN101347618A (en) | Medicament composition for treating respiratory disease | |
| CN111110634A (en) | Chloroquine phosphate inhalation aerosol and preparation method thereof | |
| CN111838743B (en) | Snuff and preparation method thereof | |
| CN109498625B (en) | Pharmaceutical composition for treating chronic obstructive pulmonary disease and preparation method thereof | |
| AU2017251548B2 (en) | Inhaled preparation of isoglycyrrhizic acid or salt thereof and use in preparing drugs for treating respiratory system diseases | |
| KR101748796B1 (en) | Inhalation capsule with enhanced delivery rate of active ingredients | |
| CN114848588A (en) | Fudosteine inhalation solution preparation and preparation method and application thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160406 |
|
| WD01 | Invention patent application deemed withdrawn after publication |